CA2633186C - 2-adamantylurea derivatives as selective 11.beta.-hsd1 inhibitors - Google Patents

2-adamantylurea derivatives as selective 11.beta.-hsd1 inhibitors Download PDF

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CA2633186C
CA2633186C CA2633186A CA2633186A CA2633186C CA 2633186 C CA2633186 C CA 2633186C CA 2633186 A CA2633186 A CA 2633186A CA 2633186 A CA2633186 A CA 2633186A CA 2633186 C CA2633186 C CA 2633186C
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adamantan
urea
phenyl
methyl
acid
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CA2633186A1 (en
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Denis Carniato
Christine Charon
Johannes Gleitz
Didier Roche
Bjoern Hock
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Merck Patent GmbH
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Merck Patent GmbH
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CA2633186A 2005-12-16 2006-11-22 2-adamantylurea derivatives as selective 11.beta.-hsd1 inhibitors Active CA2633186C (en)

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PCT/EP2006/011156 WO2007068330A1 (en) 2005-12-16 2006-11-22 2-ADAMANTYLUREA DERIVATIVES AS SELECTIVE 11β-HSD1 INHIBITORS

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Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7727978B2 (en) 2006-08-24 2010-06-01 Bristol-Myers Squibb Company Cyclic 11-beta hydroxysteroid dehydrogenase type I inhibitors
EP2125750B1 (de) 2007-02-26 2014-05-21 Vitae Pharmaceuticals, Inc. Zyklische harnstoff- und carbamat-hemmer aus 11-beta-hydroxysteroid-dehydrogenase 1
EP2172453A4 (de) 2007-06-27 2010-12-22 Taisho Pharmaceutical Co Ltd VERBINDUNG MIT 11-ß-HSD1-HEMMUNGSAKTIVITÄT
JP5451611B2 (ja) 2007-07-26 2014-03-26 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1のサイクリックインヒビター
WO2009020140A1 (ja) * 2007-08-06 2009-02-12 Dainippon Sumitomo Pharma Co., Ltd. アダマンチルウレア誘導体
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
AR069207A1 (es) 2007-11-07 2010-01-06 Vitae Pharmaceuticals Inc Ureas ciclicas como inhibidores de la 11 beta - hidroxi-esteroide deshidrogenasa 1
JP5490014B2 (ja) 2007-12-11 2014-05-14 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1型の環状尿素阻害剤
TW200934490A (en) 2008-01-07 2009-08-16 Vitae Pharmaceuticals Inc Lactam inhibitors of 11 &abgr;-hydroxysteroid dehydrogenase 1
WO2009094169A1 (en) 2008-01-24 2009-07-30 Vitae Pharmaceuticals, Inc. Cyclic carbazate and semicarbazide inhibitors of 11beta-hydroxysteroid dehydrogenase 1
JP5734666B2 (ja) 2008-02-11 2015-06-17 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の1,3−オキサアゼパン−2−オン及び1,3−ジアゼパン−2−オン阻害剤
EP2254872A2 (de) 2008-02-15 2010-12-01 Vitae Pharmaceuticals, Inc. Cycloalkyllactamderivate als inhibitoren von 11-beta-hydroxysteroiddehydrogenase 1
TW200944526A (en) * 2008-04-22 2009-11-01 Vitae Pharmaceuticals Inc Carbamate and urea inhibitors of 11β-hydroxysteroid dehydrogenase 1
JP5301563B2 (ja) 2008-05-01 2013-09-25 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状インヒビター
US8569292B2 (en) 2008-05-01 2013-10-29 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11β-hydroxysteroid dehydrogenase 1
EP2291373B1 (de) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclische inhibitoren von 11beta-hydroxysteroiddehydrogenase 1
EP2291370B1 (de) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclische inhibitoren von 11beta-hydroxysteroiddehydrogenase 1
US7863533B2 (en) * 2008-06-07 2011-01-04 Apple Inc. Cantilevered push button having multiple contacts and fulcrums
JP5777030B2 (ja) 2008-07-25 2015-09-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1の阻害剤
JP5379160B2 (ja) 2008-07-25 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状インヒビター
JP5390610B2 (ja) 2008-07-25 2014-01-15 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 11β−ヒドロキシステロイドデヒドロゲナーゼ1型の阻害剤の合成
EP2322505A4 (de) 2008-08-29 2011-10-19 Kowa Co 1-adamantylazetidin-2-on-derivat, herstellung davon und pharmazeutisches präparat damit
EP2393807B1 (de) 2009-02-04 2013-08-14 Boehringer Ingelheim International GmbH Zyklische 11beta-hydroxysteroid-dehydrogenase-1-hemmer
WO2010123838A2 (en) * 2009-04-20 2010-10-28 Abbott Laboratories Novel amide and amidine derivatives and uses thereof
MA33216B1 (fr) 2009-04-30 2012-04-02 Boehringer Ingelheim Int Inhibiteurs cycliques de la 11béta-hydroxysteroïde déshydrogénase 1
ES2350077B1 (es) 2009-06-04 2011-11-04 Laboratorios Salvat, S.A. Compuestos inhibidores de 11beta-hidroxiesteroide deshidrogenasa de tipo 1.
WO2011011123A1 (en) 2009-06-11 2011-01-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1 based on the 1,3 -oxazinan- 2 -one structure
JP5749263B2 (ja) 2009-07-01 2015-07-15 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 11β−ヒドロキシステロイドデヒドロゲナーゼ1の環状インヒビター
US8552212B2 (en) 2009-11-05 2013-10-08 Boehringer Ingelheim International Gmbh Chiral phosphorus ligands
ES2529768T3 (es) * 2009-11-11 2015-02-25 Sumitomo Dainippon Pharma Co., Ltd. Derivado 8-Azabiciclo [3.2.1] octano-8-carboxamida
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
WO2011149822A1 (en) 2010-05-26 2011-12-01 Boehringer Ingelheim International Gmbh 2-oxo-1,2-dihydropyridin-4-ylboronic acid derivatives
JP5860042B2 (ja) 2010-06-16 2016-02-16 ヴァイティー ファーマシューティカルズ,インコーポレイテッド 置換5、6及び7員複素環、そのような化合物を含有する医薬及びそれらの使用
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
US8530413B2 (en) 2010-06-21 2013-09-10 Sanofi Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments
JP5813106B2 (ja) 2010-06-25 2015-11-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 代謝障害の処置のための11−β−HSD1のインヒビターとしてのアザスピロヘキサノン
TW201215388A (en) 2010-07-05 2012-04-16 Sanofi Sa (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments
TW201215387A (en) 2010-07-05 2012-04-16 Sanofi Aventis Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament
TW201221505A (en) 2010-07-05 2012-06-01 Sanofi Sa Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament
CN103168028A (zh) 2010-09-03 2013-06-19 大日本住友制药株式会社 环酰胺衍生物
AU2011325286B2 (en) 2010-11-02 2015-04-16 Boehringer Ingelheim International Gmbh Pharmaceutical combinations for the treatment of metabolic disorders
US8710050B2 (en) 2011-03-08 2014-04-29 Sanofi Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2766349B1 (de) 2011-03-08 2016-06-01 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
KR101332805B1 (ko) 2011-03-31 2013-11-27 한국화학연구원 아다만틸기를 갖는 설파마이드 유도체 및 이의 약제학적으로 허용 가능한 염
WO2013037390A1 (en) 2011-09-12 2013-03-21 Sanofi 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors
EP2760862B1 (de) 2011-09-27 2015-10-21 Sanofi 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridin-4-carbonsäureamidderivate als kinaseinhibitoren
RU2486893C1 (ru) * 2012-06-13 2013-07-10 Федеральное государственное бюджетное образовательное учреждение высшего профессионального образования "Волгоградский государственный технический университет" (ВолгГТУ) Способ получения бис[3-метил(адамант-1-ил)]мочевин
JP6980534B2 (ja) 2015-06-25 2021-12-15 ザ チルドレンズ メディカル センター コーポレーション 造血幹細胞の増大、富化、および維持に関する方法および組成物
CN104974084A (zh) * 2015-07-19 2015-10-14 佛山市赛维斯医药科技有限公司 一类胺基二吡啶叔醇结构的11β-HSD1抑制剂及其用途
CN105085345B (zh) * 2015-08-14 2016-09-14 天津小新医药科技有限公司 含硝基的l-薄荷醇类p2y12受体拮抗剂及其用途
CN105085346B (zh) * 2015-08-14 2017-03-29 天津小新医药科技有限公司 含胺基的l-薄荷醇类p2y12受体拮抗剂及其用途
AU2017235461B2 (en) 2016-03-15 2023-02-23 Children's Medical Center Corporation Methods and compositions relating to hematopoietic stem cell expansion
EP3235813A1 (de) 2016-04-19 2017-10-25 Cidqo 2012, S.L. Aza-tetra-cyclo-derivate
RU2697409C1 (ru) * 2019-04-30 2019-08-14 Федеральное государственное бюджетное учреждение науки Новосибирский институт органической химии им. Н.Н. Ворожцова Сибирского отделения Российской академии наук (НИОХ СО РАН) 1-Адамантил-3-(((1R,4aS,10aR)-7-изопропил-1,4а-диметил-1,2,3,4,4а,9,10,10а-октагидрофенантрен-1-ил)метил)мочевина, проявляющая ингибирующее действие в отношении фермента тирозил-ДНК-фосфодиэстеразы 1 человека и увеличивающая активность темозоломида в отношении клеток глиобластомы

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3621100A (en) * 1965-11-18 1971-11-16 Geigy Chem Corp Composition and method for producing a tuberculostatic effect
US4036979A (en) * 1974-01-25 1977-07-19 American Cyanamid Company Compositions containing 4,5,6,7-tetrahydrobenz[b]thien-4-yl-ureas or derivatives and methods of enhancing growth rate
CA1060899A (en) * 1974-01-25 1979-08-21 Goro Asato Substituted tetrahydrobenzothiophenes
US4154740A (en) 1976-03-23 1979-05-15 American Cyanamid Company Substituted tetrahydrobenzothiophenes and method of preparation thereof
US4349552A (en) 1978-10-30 1982-09-14 Fujisawa Pharmaceutical Company, Ltd. 5-Fluorouracil derivatives, and their pharmaceutical compositions
FR2692575B1 (fr) 1992-06-23 1995-06-30 Sanofi Elf Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
US5292736A (en) 1993-02-26 1994-03-08 Sterling Winthrop Inc. Morpholinoalkylindenes as antiglaucoma agents
US5532237A (en) 1995-02-15 1996-07-02 Merck Frosst Canada, Inc. Indole derivatives with affinity for the cannabinoid receptor
FR2741621B1 (fr) 1995-11-23 1998-02-13 Sanofi Sa Nouveaux derives de pyrazole, procede pour leur preparation et compositions pharmaceutiques en contenant
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
AR008789A1 (es) 1996-07-31 2000-02-23 Bayer Corp Piridinas y bifenilos substituidos
WO1998041519A1 (en) 1997-03-18 1998-09-24 Smithkline Beecham Corporation Novel cannabinoid receptor agonists
JP2003514508A (ja) 1997-07-01 2003-04-15 ノボ ノルディスク アクティーゼルスカブ グルカゴン拮抗剤/逆作用剤
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
AU8127998A (en) 1997-07-11 1999-02-08 Japan Tobacco Inc. Quinoline compounds and medicinal uses thereof
AU9454098A (en) * 1997-09-24 1999-04-12 Nova Molecular, Inc. Methods for increasing apoe levels for the treatment of neurodegenerative disease
EP1085869A4 (de) 1998-06-11 2001-10-04 Merck & Co Inc Spiro piperidinderivate als melanocortinrezeptoragonisten
DE19837627A1 (de) 1998-08-19 2000-02-24 Bayer Ag Neue Aminosäureester von Arylsulfonamiden und Analoga
CN1356977A (zh) 1999-05-17 2002-07-03 诺沃挪第克公司 胰高血糖素拮抗剂/反向激动剂
WO2000074679A1 (en) 1999-06-04 2000-12-14 Merck & Co., Inc. Substituted piperidines as melanocortin-4 receptor agonists
TWI279402B (en) 1999-08-20 2007-04-21 Banyu Pharma Co Ltd Spiro compounds having NPY antagonistic activities and agents containing the same
PE20010612A1 (es) 1999-09-28 2001-07-12 Bayer Corp Agonistas del receptor 3 (r3) del peptido activador de la adenilato ciclasa de la pituitaria y su uso farmacologico
AU4929601A (en) 2000-03-23 2001-10-03 Merck & Co Inc Substituted piperidines as melanocortin receptor agonists
AU4928101A (en) 2000-03-23 2001-10-03 Merck & Co Inc Spiropiperidine derivatives as melanocortin receptor agonists
CA2437492A1 (en) 2001-02-02 2002-08-15 Yoshihiro Banno Fused heterocyclic compounds
HUP0303376A3 (en) 2001-02-28 2007-08-28 Merck & Co Inc Acylated piperidine derivatives as melanocortin-4 receptor agonists, and pharmaceutical compositions containing them and use thereof
CA2422708C (en) 2001-03-22 2010-10-26 Solvay Pharmaceuticals B.V. 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity
US6573287B2 (en) 2001-04-12 2003-06-03 Bristo-Myers Squibb Company 2,1-oxazoline and 1,2-pyrazoline-based inhibitors of dipeptidyl peptidase IV and method
FR2824825B1 (fr) 2001-05-15 2005-05-06 Servier Lab Nouveaux derives d'alpha-amino-acides, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004535433A (ja) 2001-06-20 2004-11-25 メルク エンド カムパニー インコーポレーテッド 糖尿病治療用のジペプチジルペプチダーゼ阻害薬
US20020196006A1 (en) 2001-06-21 2002-12-26 Champion Microelectronic Corp. Volt-second balanced PFCPWM power converter
JP2004530729A (ja) 2001-06-27 2004-10-07 プロバイオドラッグ アーゲー ジペプチジルペプチダーゼiv触媒作用の拮抗調節に有用なペプチド構造
WO2003002530A2 (en) 2001-06-27 2003-01-09 Smithkline Beecham Corporation Pyrrolidines as dipeptidyl peptidase inhibitors
ES2291477T3 (es) 2001-06-27 2008-03-01 Smithkline Beecham Corporation Fluoropirrolidinas como inhibidores de dipeptidil peptidasa.
CN1723196A (zh) 2001-06-27 2006-01-18 史密丝克莱恩比彻姆公司 作为二肽酶抑制剂的氟代吡咯烷
ATE388951T1 (de) 2001-07-03 2008-03-15 Novo Nordisk As Dpp-iv-inhibierende purin-derivative zur behandlung von diabetes
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
WO2003007887A2 (en) 2001-07-20 2003-01-30 Merck & Co., Inc. Substituted imidazoles as cannabinoid receptor modulators
US6977264B2 (en) 2001-07-25 2005-12-20 Amgen Inc. Substituted piperidines and methods of use
EP1474139B1 (de) 2002-02-01 2007-11-21 Merck & Co., Inc. 11-beta-hydroxysteroid-dehydrogenase-1-hemmer zur behandlung von diabetes, adipositas und dyslipidämie
AR038967A1 (es) 2002-03-18 2005-02-02 Solvay Pharm Bv Derivados de 2,3 - diaril - pirazolidinas como inhibidores de enzimas que degradan la neurotensina
US20040014422A1 (en) 2002-07-19 2004-01-22 Nokia Corporation Method and system for handovers using service description data
EP1402887A1 (de) * 2002-09-18 2004-03-31 Jerini AG Neue Verbindungen zur Hemmung von unerwünschter Zellproliferation sowie deren Verwendung
AU2003269242A1 (en) 2002-10-11 2004-05-04 Astrazeneca Ab 1,4-disubstituted piperidine derivatives and their use as 11-betahsd1 inhibitors
AU2003276458A1 (en) 2002-11-07 2004-06-07 Astrazeneca Ab 2-oxo-ethanesulfonamide derivates
WO2004056744A1 (en) * 2002-12-23 2004-07-08 Janssen Pharmaceutica N.V. Adamantyl acetamides as hydroxysteroid dehydrogenase inhibitors
TW200503994A (en) 2003-01-24 2005-02-01 Novartis Ag Organic compounds
JP2006522747A (ja) 2003-04-11 2006-10-05 ノボ ノルディスク アクティーゼルスカブ 縮合1,2,4−トリアゾールの薬学的使用
ATE467616T1 (de) 2003-04-11 2010-05-15 High Point Pharmaceuticals Llc Verbindungen mit aktivität an der 11beta- hydroxasteroiddehydrogenase

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US8188288B2 (en) 2012-05-29
DK1960352T3 (da) 2013-10-28
EP1960352B1 (de) 2013-08-07
IL192053A0 (en) 2008-12-29
WO2007068330A1 (en) 2007-06-21
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KR20080079317A (ko) 2008-08-29
AR058546A1 (es) 2008-02-13
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KR101394586B1 (ko) 2014-05-12
AU2006326703B2 (en) 2012-02-23
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